• Title/Summary/Keyword: anti-thrombin activity

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Anti-coagulation and Anti-platelet Aggregation Activity of the Mature Fruit of Sorbus commixta (성숙 마가자의 혈액 응고저해 및 혈소판 응집저해 활성)

  • Kim, Mi-Sun;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
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    • v.43 no.4
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    • pp.373-377
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    • 2015
  • The mature fruit of Sorbus commixta is known as magaja in Korea and is consumed in the form of tea and wine. In addition, it has been used to treat hypertension and articular neuralgia in folk medicine. In this study, the ethanol extract of magaja and its subsequent organic solvent fractions were prepared, and their in vitro anti-coagulation, and platelet aggregation inhibitory activities were evaluated. Among the fractions, the ethylacetate fraction demonstrated significant inhibition against thrombin, prothrombin, blood coagulation factors and platelet aggregation, without hemolysis activity up to 0.5 mg/ml. Our results suggest that the ethylacetate fraction of magaja has the potential to be used as a new anti-coagulation agent.

Anti-thrombosis Activities of the Root Extract of Moringa oleifera Lam (모링가 지하부의 항혈전 활성)

  • Kwon, Chong Suk;Sung, Hwa-Jung;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
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    • v.47 no.1
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    • pp.20-24
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    • 2019
  • Moringa oleifera Lam (MOL) has been used as a traditional medicine to treat various cancers and inflammation. Whereas the bioactivities of the MOL leaf and seed are well reported, the study of the root is still rudimentary. In this study, the ethanol extract of MOL (EEMOL) and its subsequent organic solvent fractions were prepared and their anticoagulation activity in vitro and platelet aggregation inhibitory activity were evaluated. The EEMOL had negligible anticoagulation and strong platelet aggregation activities. However, the hexane and ethyl acetate fractions of EEMOL showed significant inhibition against thrombin, prothrombin, coagulation factors, and platelet aggregation, without hemolytic activity up to 1.0 mg/ml. Our results suggest that the active fractions of MOL root have potential as new anti-thrombosis agents.

Inhibitory Effects of Ginsenoslde $Rg_3$ on Platelet Aggregation and its Mechanism of Action (Ginsenoside $Rg_3$의 혈소판 응집 억제 효과 및 그 작용기전에 관한 연구)

  • 이소라;박정일
    • Journal of Ginseng Research
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    • v.21 no.2
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    • pp.132-140
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    • 1997
  • The effects of ginsenosides purified from red ginseng on platelet aggregation were investigated. Preincubation of washed platelets from rats with either ginsenoside Rg3, ginsenosides non-polar fraction (G-NPF), ginsenoside Rg1(Rg1) or ginsenosides polar fraction(G-PF) reduced the plytelet aggrelation induced by collagen in a dose-dependent manner, whereas ginsenoside Rg2 failed to inhibit the aggregation. Their IC50 values of Rg3, G-NPF, Rgl, and G-PF were 8.7$\pm$1.0, 150.3$\pm$0.1, 369.9$\pm$ 1.0, 606.211.3 $\mu\textrm{g}$/ml, respectively. Aggrelation induced by thrombin was also inhibited by Rg3 and G-NPF with IC50 being 5.2$\pm$ 1.1 and 66.5$\pm$0.8 $\mu\textrm{g}$/ml, respectively. The alterations of Intracellular Ca2+ concentration in platelets were monitored using fura-2 as a fluorescent Ca2+ indicator. Both Ca2+ release from internal stores and Ca2+ influx into cytosol were suppressed by Rg3. Rg3 also inhibited granular release of ATP and TXA2 formation induced by thrombin in a dose-dependent manner in the washed platelets. Rg3 also inhibited Aggregation and ATP release from human platelets induced by collagen to a similar extent as were observed in rat platelets. In conclusion, Rg3 is a Potent anti-aggregating component in ginsenosides and may exert its anti-aggrega1ing activity by decreasing TXAa formation and granular secretion in platelets, most likely by inhibiting Ca2+ influx and Ca2+ mobilization from intracellular stores. Thus ginseng may contribute to the prevention and treatment of thrombosis.

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Anti-microbial and Anti-thrombosis Activities of Lees of Sweet Potato Soju (고구마 소주 주박의 항균 및 항혈전 활성)

  • Kim, Mi-Sun;Lee, Ye-Seul;Kim, Jong Sik;Shin, Woo-Chang;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
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    • v.42 no.3
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    • pp.258-266
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    • 2014
  • Sweet potato soju (SPS), a form of traditional distilled alcoholic liquor in Korea, is manufactured by the distillation of fermented broth under normal pressure, thus providing it for a uniquely smooth taste infused with the flavor of sweet potato. After distillation, the lees of SPS is produced as by-product and discarded. In this study, the ethanol and hot water extracts of lees of SPS, and their subsequent organic solvent fractions using hexane, ethylacetate (EA), butanol, and water residue were prepared in an effort at the efficient re-use of the lees of SPS. The ethanol extraction yield was 1.36-fold higher than that of the hot water extraction, and the EA fraction revealed the highest total polyphenol content among the solvent fractions. The various extracts and solvent fractions did not demonstrate hemolytic activity at up to 0.5 mg/ml concentrations against human red blood cells. In the bioactivity assay, only the EA fraction displayed a broad spectrum of anti-microbial activity against different pathogenic and food spoilage bacteria, and demonstrated significant anti-coagulation activity by inhibitions of thrombin, prothrombin and blood coagulation factors. Furthermore, only the EA fraction from the hot water extract of the lees of SPS showed anti-platelet aggregation activity, which is comparable to aspirin (a commercially available drug). Our results suggest that the EA fraction of the hot water extract prepared from the lees of SPS has a high potential as a novel resource for anti-microbial and anti-thrombosis agents.

Evaluation of Antioxidant, Anti-Inflammatory, Antithrombotic, and Antiobesity Activities in Cultured Edible Plants to Increase Farm Income (농가소득 창출을 위한 식용식물의 항산화, 항염, 항혈전 및 항비만 효과 탐색)

  • Lee, Seon-Hye;Kim, Nam-Seok;Choi, Bong-Kyoum;Park, Yeon-Hee;Kim, Jung-Bong;Jang, Hwan-Hee;Hwang, Yu-Jin;Choe, Jeong-Sook;Lee, Sung-Hyen
    • The Korean Journal of Community Living Science
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    • v.28 no.1
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    • pp.29-43
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    • 2017
  • We studied the antioxidant, the anti-inflammatory, antithrombotic, and antiobesity activities of seven different kinds of edible plants. 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ABTS radical scavenging activities were determined as a measurement of antioxidant activity. NO production inhibition by the macrophage cell line (Raw 264.7) treated with lipopolysaccharide (LPS) was carried out to assess anti-inflammatory activity. Thrombin inhibitory activity was measured for its antithrombotic function and inhibition of 3T3-L1 cell differentiation was evaluated as a measurement of antiobesity activity. Total phenolic components and total flavonoid contents were measured to determine functional materials in medicinal plants. Common sage, Japanese lady bell, and hairy agrimony showed high antioxidant activity ($IC_{50}$) of less than $100{\mu}g/mL$. All samples used in this study showed anti-inflammatory activity. Common sage, hairy agrimony, and hooker chives showed antithrombotic effects. Hairy agrimony showed the highest antithrombotic effect (98.1%). Common sage, Japanese lady belly, hairy agrimony, and hooker chives showed reduced 3T3-L1 cell differentiation and hooker chives strongly inhibited lipid accumulation in the cells compared to other medicinal plants. Common sage and hairy agrimony contained more than 1 mg GAE/g of phenolic compounds and more than 1 mg CE/g of flavonoids. Functional activities were different by plant part and extraction method from each sample. These results suggest that common sage, Japanese lady belly, hairy agrimony, and hooker chives may be used as healthy food sources with antioxidant, anti-inflammatory, antithrombotic, and antiobesity activities, and appropriate extracting methods from each plant need to be developed.

Evaluation of Useful Biological Activities of Hot-Water Extracts of Raw-Red Bean and Boiled-Red Bean (Phaseolus radiatus L.) (생팥 및 삶은 팥의 열수 추출물의 유용 생리활성 평가)

  • Jung, In-Chang;Lee, Ye-Seul;Kang, Dong-Kyoon;Sohn, Ho-Yong
    • Journal of the East Asian Society of Dietary Life
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    • v.25 no.3
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    • pp.451-459
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    • 2015
  • Raw-red bean (RR) should be boiled in hot water, and only boiled-red bean (BR) has been used in the food industry. In the course of development of functional food using red- bean (Phaseolus radiatus L), hot- water extracts (HWEs) of RR and BR were prepared, respectively and their components and various biological activities were compared. The extraction yield at $100^{\circ}C$ of RR (16.2%) was higher than that of BR (14.8%), and contents of total polyphenols, total flavonoids and reducing sugars of HWE of RR were 2.5-fold, 2.1-fold and 1.5-fold higher than those of HWE of BR. In anti-oxidation activity assay, scavenging activities against DPPH anion and ABTS cation as well as reducing power of RR was higher than those of BR. The results suggest that the anti-oxidant compounds in red bean might be heat-liable or discarded during boiling in hot-water as a cooking drip. Unexpectedly, nitrite scavenging activity was stronger in HWE of BR than RR. In anti-microbial activity assay, HWE of RR ($500{\mu}g/disc$) showed growth inhibition activity against gram-positive bacteria, whereas HWE of BR did not show any activity against any tested bacteria and fungi. Assay of in-vitro anti-diabetes and anti-thrombosis activities, which were previously reported in ethanol extract of red-bean, revealed that HWEs of RR and BR did not show significant activities against ${\alpha}$-amylase, ${\alpha}$-glucosidase, thrombin, prothrombin, or blood coagulation factors. Our results suggest that the anti-oxidation, anti-diabetes and anti-thrombosis activities of HWEs of RR and BR were lower than those of ethanol extracts of red bean, and bioactive substances in RR were destroyed during boiling or discarded after boiling. Further research on suitable boiling and re-use of cooking drip of red bean is necessary.

Anti-coagulation and Anti-platelet Aggregation Activities of Black Ginger (Kaempferia parviflora) (흑생강(Kaempferia parviflora)의 항응고 및 혈소판 응집저해 활성)

  • Lee, Man-Hyo;Sung, Hwa-Jung;Kwon, Chong Suk;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.28 no.9
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    • pp.1068-1075
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    • 2018
  • Kaempferia parviflora, an herbaceous plant in the family Zingiberaceae, is popular in many tropical regions. It is called as black ginger or krachaidum in Thailand and Laos, and its raw or dried root have been used as spices and teas. The rhizomes also have been traditionally used to treat gastrointestinal disorders, ulcers, gout, dysentery, allergies and to improve physical work capacity. Recently, its anti-obesity, anti-oxidant, anti-inflammatory and blood clot-lysis activities were reported. In this study, the anti-thrombosis activity of black ginger was investigated, since improvement in blood fluidity leads to the prevention of various lifestyle-related diseases. The hot water and ethanol extract and their subsequent solvent fractions (hexane, ethylacetate, butanol fractions and water residue) were prepared, and their anti-coagulation and platelet aggregation inhibitory activities were determined, respectively. Among the black ginger extracts and their fractions, the ethylacetate fraction (EAF) of ethanol extract only showed significant extensions of blood coagulation time determined by thrombin time (TT), prothrombin time (PT), and activated partial thromboplastin time (aPTT). At 5 mg/ml concentration, TT, PT and aPTT were extended to 1.22, 1.49 and >15-folds compared to non-treatment. The EAFs of ethanol and hot water extract showed strong inhibitions against collagen-induced platelet aggregations, which are comparable to inhibitions of aspirin. Also the EAFs from black ginger did not show any hemolysis activity against human RBC up to 0.5 mg/ml. Our results suggest that the EAF of black ginger has a potential as novel anti-coagulation and ant-platelet aggregation agent. This report provides the first evidence of anti-coagulation activity of black ginger.

Evaluation of Antimicrobial, Antithrombin, and Antioxidant Activity of Dioscorea batatas Decne (마(Dioscorea batatas Decne)의 항균, 항산화 및 항혈전 활성 평가)

  • Kim, Jee-In;Jang, Han-Su;Kim, Jong-Sik;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
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    • v.37 no.2
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    • pp.133-139
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    • 2009
  • Yam (Dioscorea batatas Decne) has been recognized as healthy food due to its various biological activities, such as anti-obesity, anti-constipation, anti-proliferation, anti-mutagenic activity, and decrease of blood glucose and cholesterol level. In this study, the methanol extract and its organic solvent fractions were prepared from dried Dioscorea batatas Decne, and their antimicrobial, antithrombin, and antioxidant activity were evaluated, respectively. The 66.7% of methanol extract was fractioned into water residue, and most of total-polyphenol/total-flavonoids were found in ethylacetate fraction. This ethylacetate fraction at $500\;{\mu}g/disc$ concentration showed strong antibacterial activity against gram-negative and gram-positive bacteria, except Staphylococcus aureus. Antifungal activity was not observed in methanol extract and its fractions. But, strong antithrombin activity was found in methanol extract. At 4.8 mg/mL concentration, thrombin time was 99.5 sec, which is coincides with 30% activity of aspirin, a commercial available antithrombosis agent. The ethylacetate fraction showed strong DPPH scavenging activity ($IC_{50}$ of $80.5\;{\mu}g/mL$), compared to vitamin C ($IC_{50}$ of $15.2\;{\mu}g/mL$). Also, the ethylacetate fraction showed strong SOD-like activity and reducing power, which are coincide with 43% of vitamin C and 82.7% of butylated hydroxytoluene activity, respectively.

Effect of Antibiotics upon the Antibacterial Activity of Platelet Microbicidal Protein against Streptococcus rattus BHT

  • Kim, Jae-Wook;Choe, Son-Jin;Lee, Si-Young
    • International Journal of Oral Biology
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    • v.34 no.1
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    • pp.43-48
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    • 2009
  • Thrombin-induced platelet microbicidal protein (tPMP) is a small cationic peptide that exerts potent in vitro microbicidal activity against a broad spectrum of human pathogens, including Staphylococcus aureus and Streptococcus rattus BHT. Earlier evidence has suggested that tPMP targets and disrupts the bacterial membrane. However, it is not yet clear whether membrane disruption itself is sufficient to kill the bacteria or whether subsequent, presumably intracellular, events are also involved in this process. In this study, we investigated the microbicidal activity of rabbit tPMP toward S. rattus BHT cells in the presence or absence of a pretreatment with antibiotics that differ in their mechanisms of action. The streptocidal effects of tPMP on control cells (no antibiotic pretreatment) were rapid and concentration-dependent. Pretreatment of S. rattus BHT cells with either penicillin or amoxicillin (inhibitors of bacterial cell wall synthesis) significantly enhanced the anti-S. rattus BHT effects of tPMP compared with the effects against the respective control cells over most tPMP concentration ranges tested. On the other hand, pretreatment of S. rattus BHT cells with tetracycline or doxycycline (30S ribosomal subunit inhibitors) significantly decreased the streptocidal effects of tPMP over a wide peptide concentration range. Furthermore, pretreatment with rifampin (an inhibitor of DNA-dependent RNA polymerase) essentially blocked the killing of S. rattus BHT by tPMP at most concentrations compared with the respective control cells. These results suggest that tPMP exerts anti-S. rattus BHT activity through mechanisms involving both the cell membrane and intracellular targets.

A study on anti-thrombotic activity of Hwao-tang

  • Park Tae Woo;Park Won Hwan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.1
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    • pp.181-185
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    • 2002
  • The thrombosis is the category of blood stasis. Blood stasis is a pathologicial state resulting from the reverse or impeded flow of blood in the body or the stagnation of blood flow in local parts as well as abnormal blood outside of the vessles which remains in the body and fails to disperse. Hwao-tang has been reported to have a hypolipidemic effect in patients with hypercholesterolemia, and in highcholesterol-induced experimental models. The present paper reports the effects of HOT on atherosclerosis using a spontaneous experimental model, Kurosawa and Kusanagi-hypercholesterolemic (KHC) rabbits. We have also investigated the pharmacological effect of extracts obtained from HOT on collagen-and ADP-induced blood platelet aggregation, thrombin-induced conversion of fibrinogen and fibrinolysis in in vitro experiments. In conclusion, the protection of extracts of Korean herbs' HOT on the ischemic infarction induced artificially might be involved to their inhibition of thrombotic action.